Cell growth is dramatically reduced by lignocaine (10 nM; 48 hours) [2]. Cell viability is inhibited by lidocaine (1-10 nM; 24-72 hours); the maximum inhibitory effect is obtained at a dose of 10 nM and a treatment duration of 48 hours [2]. The rate of apoptosis is markedly increased by lidocaine (10 nM; 48 hours) [2]. Lidocaine (10 nM; 48 hours) dramatically increases the expression of p21 and downregulates Cyclin D1 [2].

In rats, lidocaine (lidocaine) produces a completely reversible block of the tail nerve. Compared to thermal nociceptive blockade, mechanical nociceptive blockade, which is generated by lidocaine, has a slower onset and a quicker recovery [3].

Cell proliferation experiment [2]
Cell Types: human gastric cancer cell line MKN45
Tested Concentrations: 10 nM
Incubation Duration: 48 hrs (hours)
Experimental Results: Cell proliferation diminished Dramatically.

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Cell viability assay [2]
Cell Types: human gastric cancer cell line MKN45
Tested Concentrations: 1, 5 and 10 nM
Incubation Duration: 24, 48, 72 hrs (hours)
Experimental Results: Inhibition of MKN45 cell viability.

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Cell apoptosis analysis [2]
Cell Types: Human gastric cancer cell line MKN45
Tested Concentrations: 10 nM
Incubation Duration: 48 hrs (hours)
Experimental Results: The cell apoptosis rate increased Dramatically.

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Western Blot Analysis [2]
Cell Types: human gastric cancer cell line MKN45
Tested Concentrations: 10 nM
Incubation Duration: 48 hrs (hours)
Experimental Results: Cyclin D1 expression was Dramatically down-regulated, and p21 expression was Dramatically up-regulated.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Lidocaine concentrations in breast milk are low with continuous intravenous infusion, epidural administration, and high-dose local anesthesia, and infants do not absorb lidocaine well. Lidocaine is not expected to have any adverse effects on breastfed infants. No special precautions are required.
There have been reports that lidocaine used in combination with other anesthetics and analgesics during labor may interfere with breastfeeding. However, this assessment is controversial and complex due to the large number of drug combinations, dosages, and patient populations involved in studies, the variety of techniques used, and flawed study designs. Overall, with good breastfeeding support, epidural lidocaine has little or no adverse effect on the success of breastfeeding, whether in combination with fentanyl or its derivatives. Labor analgesia may delay the onset of lactation.
◉ Effects on Breastfed Infants
During delivery, the administration of 60 to 500 mg of lidocaine to mothers via intrapleural or epidural routes had no effect on 14 infants (including both breastfed and bottle-fed infants).
A neurology team reported that they administered peripheral nerve blocks using 1% lidocaine to 14 lactating mothers with migraines. They reported no adverse effects on the infants and considered the procedure safe during breastfeeding.
◉ Effects on Lactation and Breast Milk
A randomized study compared three groups of women undergoing elective cesarean sections who received a subcutaneous infusion of 20 ml of 1% lidocaine plus 1:100:000 epinephrine at the incision site. One group received lidocaine before the incision, one group received lidocaine after the incision, and the third group received 10 ml of lidocaine both before and after the incision. Women who received lidocaine both before and after the incision started breastfeeding earlier than those who received lidocaine before the incision (3.4 hours vs. 4.1 hours). Women who received lidocaine after the incision showed no difference in the time to breastfeeding initiation compared to the other two groups. A national survey of women from late pregnancy to 12 months postpartum compared the time to lactation stage II in mothers who received and did not receive analgesia during labor. Drug classes included: spinal or epidural anesthesia alone, spinal or epidural anesthesia combined with other drugs, and other analgesics alone. Women who received any class of drugs were approximately twice as likely to experience delayed lactation stage II (>72 hours) as women who did not receive labor analgesia. An Egyptian study compared the effects of 2% lidocaine (n=75) and 2% lidocaine plus 1:200,000 epinephrine (n=70) in wound infiltration anesthesia after cesarean section. Patients receiving lidocaine combined with epinephrine anesthesia were able to begin breastfeeding 89 minutes post-surgery, while those receiving lidocaine anesthesia alone required 132 minutes. This difference was statistically significant.

[1]. Setting up for the block: the mechanism underlying lidocaine's use-dependent inhibition of sodium channels. J Physiol. 2007 Jul 1;582(Pt 1):11.

[2]. Lidocaine inhibits growth, migration and invasion of gastric carcinoma cells by up-regulation of miR-145. BMC Cancer. 2019 Mar 15;19(1):233.

[3]. Evaluation of the antinociceptive effects of lidocaine and bupivacaine on the tail nerves of healthy rats. Basic Clin Pharmacol Toxicol. 2013 Jul;113(1):31-6.

Lidocaine hydrochloride is the hydrochloride salt form of lidocaine, an aminoacetamide drug and a typical representative of amide anesthetics. Lidocaine interacts with voltage-gated sodium ion channels on nerve cell membranes, blocking the transient increase in sodium ion permeability to the excitatory membrane. This prevents the generation and conduction of nerve impulses, leading to reversible sensory loss. Lidocaine hydrochloride also has class IB antiarrhythmic activity. It reduces sodium ion inflow into myocardial tissue, especially the Purkinje fiber network, during phase 0 of the action potential (i.e., phase 0 of the cardiac cycle), thereby reducing depolarization, automaticity, and excitability. It is a local anesthetic and cardiac depressant used as an antiarrhythmic agent. Its potency and duration of action are stronger than procaine, but its duration of action is shorter than bupivacaine or prilocaine. See also: Lidocaine hydrochloride (note moved to).

C14H25CLN2O2

288.816

288.16

6108-05-0

Lidocaine;137-58-6

16219577

White to off-white solid powder

350.8ºC at 760 mmHg

68.5ºC

166ºC

3.394

3

3

5

19

228

0

O=C(C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])N([H])C1C(C([H])([H])[H])=C([H])C([H])=C([H])C=1C([H])([H])[H]

YECIFGHRMFEPJK-UHFFFAOYSA-N

InChI=1S/C14H22N2O.ClH/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4;/h7-9H, 5-6,10H2,1-4H3,(H,15,17);1H;

2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide;hydrate;hydrochloride;

Lidocaine Hydrochloride; LIDOCAINE HCL; Lidothesin; Lignocaine hydrochloride; Xyloneural; Xylocitin;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)